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CVT-10216

SKU: orb1308421

Description

CVT-10216

Research Area

Metabolism Research

Images & Validation

Key Properties

CAS Number1005334-57-5
MW465.48
Purity99.16%
FormulaC24H19NO7S
SMILESCS(=O)(=O)Nc1ccc(cc1)-c1coc2cc(OCc3cccc(c3)C(O)=O)ccc2c1=O
TargetDehydrogenase
SolubilityDMF:25 mg/mL (53.71 mM);DMSO:20 mg/mL (42.97 mM);10% DMSO+90% Corn Oil:2 mg/mL (4.3 mM)

Bioactivity

Target IC50
ALDH2:29 nM
In Vivo
CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 that reduces excessive alcohol drinking. Anxiety plays a role in alcoholism. As reflected in social interaction behavior in four unrelated rodent models: endogenous anxiety-like behavior in na ve Fawn-Hooded rats, repeated alcohol-withdrawal-induced anxiety, restraint stress-induced anxiety and drug-induced anxiety. CVT-10216 counteracted anxiety in all models except that produced by the 5-HT(2C) agonist, mCPP. CVT-10216 exhibited both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety. Importantly, anxiogenic behavior induced by the benzodiazepine receptor inverse agonist, DMCM, was counteracted dose-dependently by CVT-10216.CVT-10216 (intraperitoneal injection; 3.75 or 15 mg/kg) are determined 5 h into the third withdrawal, it has the anxiolytic effect of 15 mg/kg CVT-10216 in this model. However it has no significant effects on locomotor activity. CVT-10216 (intraperitoneal injection; 3.75, 7.5, or 15 mg/kg) shows a increase in social interaction as a dose-dependent manner, punctuated by a 2-fold increase in social interaction after 15 mg/kg in Fawn-Hooded rats.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

social, CVT-10216, CVT10216, CVT 10216, ALDH2, ALDH-2, Aldehyde Dehydrogenase (ALDH), ALDH, alcohol-preferring, anxiolytic, inhibit, interaction, Inhibitor
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Key Properties

No computed properties available.

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Protocol Information

CVT-10216 (orb1308421)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 90.00
5 mg
$ 140.00
1 ml x 10 mM (in DMSO)
$ 160.00
10 mg
$ 220.00
25 mg
$ 400.00
50 mg
$ 610.00
100 mg
$ 860.00
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